ABT-639，50MG，SML4099-50MG，Sigma

Biochem/physiol Actions

Orally active, peripherally acting, potent and Cav3.2-selective T-type calcium channel blocker with antinociception efficacy in vivo.

ABT-639 is an orally active, peripherally acting, potent and Cav3.2-selective T-type calcium channel blocker (hCav3.2 IC50 = 2 μM vs. >30 μM against Cav3.1/Cav3.3) that attenuates low-voltage-activated (LVA) currents in rat DRG neurons (IC50 = 7.6 μM). ABT-639 exhibits antinociception efficacy in a rat knee joint pain model (ED50 = 2 mg/kg, p.o.), and increases tactile allodynia thresholds in multiple models of neuropathic pain in vivo (10-100 mg/kg, p.o.) with no adverse effects on hemodynamic or psychomotor function even at doses as high as 300 mg/kg.